Compounds > sk&f 96067
Page last updated: 2024-12-10

sk&f 96067

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

3-butyryl-4-(2-methylphenylamino)-8-methoxyquinoline: reversible, lumenally acting inhibitor of the gastric H(+)+ K(+))-ATPase; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID3081087
CHEMBL ID327717
SCHEMBL ID451221
MeSH IDM0190139

Synonyms (21)

Synonym
CHEMBL327717 ,
sk-96067
skf-96067
115607-61-9
1-butanone, 1-(8-methoxy-4-((2-methylphenyl)amino)-3-quinolinyl)-
3-butyryl-4-(2-methylphenylamino)-8-methoxyquinoline
sk&f-96067
sk&f 96067
1-[8-methoxy-4-(2-methylanilino)quinolin-3-yl]butan-1-one
1-(8-methoxy-4-o-tolylamino-quinolin-3-yl)-butan-1-one
bdbm50001254
SCHEMBL451221
MAVJDLHBPIXVJL-UHFFFAOYSA-N ,
DTXSID40151146
skf96067
HY-U00042
CS-6768
AKOS030618286
1-butanone, 1-[8-methoxy-4-[(2-methylphenyl)amino]-3-quinolinyl]-
3-butyryl-8-methoxy-4-[(2-methylphenyl)amino]quinoline
SB72126

Research Excerpts

Dosage Studied

ExcerptRelevanceReference
" From this series, compound 17c (SK&F 96067) was shown to be a potent inhibitor of histamine-stimulated gastric acid secretion after oral dosing in the Heidenhain pouch dog and was selected for further development and evaluation in man."( Reversible inhibitors of the gastric (H+/K+)-ATPase. 3. 3-substituted-4-(phenylamino)quinolines.
Brown, TH; Ife, RJ; Keeling, DJ; Leach, CA; Meeson, ML; Parsons, ME; Reavill, DR; Theobald, CJ; Wiggall, KJ, 1992)		0.56
" In this model, duration of action studies showed that significant residual inhibition of acid secretion remained 8 hours after intravenous dosing with SK&F 97574 (producing peak inhibition of 92%)."( Properties of the reversible, K(+)-competitive inhibitor of the gastric (H+/K+)-ATPase, SK&F 97574. II. Pharmacological properties.
Ife, RJ; Leach, C; Parsons, ME; Pope, AJ; Postius, S; Rasmussen, TC; Rushant, B, 1995)		0.29
" Some compounds also proved to be effective inhibitors of stimulated acid secretion in both the rat and dog when dosed intravenously."( Reversible inhibitors of the gastric (H+/K+)-ATPase. 5. Substituted 2,4-diaminoquinazolines and thienopyrimidines.
Blurton, P; Brown, TH; Ife, RJ; Keeling, DJ; Leach, CA; Meeson, ML; Parsons, ME; Theobald, CJ, 1995)		0.29
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (12)

Assay IDTitleYearJournalArticle
AID32536Concentration required to inhibit the activity of K+ stimulated gastric ATPase1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Reversible inhibitors of the gastric (H+/K+)-ATPase. 3. 3-substituted-4-(phenylamino)quinolines.
AID178227Inhibition of pentagastrin-stimulated gastric acid secretion in the anesthetized rat after iv administration1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Reversible inhibitors of the gastric (H+/K+)-ATPase. 4. Identification of an inhibitor with an intermediate duration of action.
AID176170Compound was tested in vivo for gastric antisecretory activity after 5 hr of pylorus ligation of SD rat1999Bioorganic & medicinal chemistry letters, Oct-04, Volume: 9, Issue:19
Synthesis and pharmacological profile of 1-aryl-3-substituted pyrrolo[3,2-c]quinolines.
AID78892Inhibition of K+ -stimulated gastric ATPase activity was measured using lyophilized gastric vesicles at pH 71995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Reversible inhibitors of the gastric (H+/K+)-ATPase. 4. Identification of an inhibitor with an intermediate duration of action.
AID59999Inhibition of histamine stimulated gastric acid secretion was tested in heidenhain pouch dog upon intravenous administration1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Reversible inhibitors of the gastric (H+/K+)-ATPase. 3. 3-substituted-4-(phenylamino)quinolines.
AID177087Inhibition of pentagastrin stimulated gastric acid secretion in anesthetized rat upon intravenous administration1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Reversible inhibitors of the gastric (H+/K+)-ATPase. 3. 3-substituted-4-(phenylamino)quinolines.
AID60746Mean percent peak inhibition of histamine-stimulated gastric acid secretion in the heidenhain pouch dog following a single dose of 1 umol/kg through iv administration.1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Reversible inhibitors of the gastric (H+/K+)-ATPase. 4. Identification of an inhibitor with an intermediate duration of action.
AID60393Histamine-stimulated gastric acid secretion in Heidenhain pouch dog at 4uM/Kg, on iv administration of the compound1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Reversible inhibitors of the gastric (H+/K+)-ATPase. 5. Substituted 2,4-diaminoquinazolines and thienopyrimidines.
AID78907Compound was tested in vitro for H+/K+ ATPase activity in rabbit stomach preparations1999Bioorganic & medicinal chemistry letters, Oct-04, Volume: 9, Issue:19
Synthesis and pharmacological profile of 1-aryl-3-substituted pyrrolo[3,2-c]quinolines.
AID60748Mean percent peak inhibition of histamine-stimulated gastric acid secretion in the heidenhain pouch dog following a single dose of 4 umol/kg through oral administration.1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Reversible inhibitors of the gastric (H+/K+)-ATPase. 4. Identification of an inhibitor with an intermediate duration of action.
AID60000Inhibition of histamine stimulated gastric acid secretion was tested in heidenhain pouch dog upon oral administration1992Journal of medicinal chemistry, Sep-04, Volume: 35, Issue:18
Reversible inhibitors of the gastric (H+/K+)-ATPase. 3. 3-substituted-4-(phenylamino)quinolines.
AID60392Histamine-stimulated gastric acid secretion in Heidenhain pouch dog at 1uM/Kg, on iv administration of the compound1995Journal of medicinal chemistry, Jul-07, Volume: 38, Issue:14
Reversible inhibitors of the gastric (H+/K+)-ATPase. 5. Substituted 2,4-diaminoquinazolines and thienopyrimidines.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (9)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's9 (100.00)18.2507
2000's0 (0.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.15

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.15 (24.57)
Research Supply Index2.30 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.15)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (11.11%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (88.89%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
cimetidine
Cimetidine: A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.. cimetidine : A member of the class of guanidines that consists of guanidine carrying a methyl substituent at position 1, a cyano group at position 2 and a 2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl group at position 3. It is a H2-receptor antagonist that inhibits the production of acid in stomach.		2.3920aliphatic sulfide;
guanidines;
imidazoles;
nitrile		adjuvant;
analgesic;
anti-ulcer drug;
H2-receptor antagonist;
P450 inhibitor
omeprazole
Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.		2.6830aromatic ether;
benzimidazoles;
pyridines;
sulfoxide
acridine orange
Acridine Orange: A cationic cytochemical stain specific for cell nuclei, especially DNA. It is used as a supravital stain and in fluorescence cytochemistry. It may cause mutations in microorganisms.. acridine orange : Fluorescent dye useful for cell cycle determination. It is cell-permeable, and interacts with DNA and RNA by intercalation or electrostatic attractions respectively.. acridine orange free base : A member of the class of aminoacridines that is acridine carrying two dimethylamino substituents at positions 3 and 6. The hydrochloride salt is the fluorescent dye 'acridine orange', used for cell cycle determination.		1.9710aminoacridines;
aromatic amine;
tertiary amino compound		fluorochrome;
histological dye
sch 28080
Sch 28080: not related structurally to other known anti-ulcer agents; inhibits histamine-stimulated gastric secretion; prevents gastric lesions induced by aspirin, indomethacin & ethanol		3.7730imidazopyridine
sk&f-96356
1-(2-methylphenyl)-4-methylamino-6-methyl-2,3-dihydropyrrolo(3,2-c)quinoline: a K+-competitive fluorescent inhibitor of the H,K-ATPase; structure given in first source		1.9810
ConditionIndicatedRelationship StrengthStudiesTrials
Gastric Ulcer
[description not available]		0210
Stomach Ulcer
Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).		0210
Gastric Fistula
Abnormal passage communicating with the STOMACH.		01.9810
Bone Loss, Osteoclastic
[description not available]		01.9810
Muscle Relaxation
That phase of a muscle twitch during which a muscle returns to a resting position.		01.9910